2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. 5-HT Receptor Histamine Receptor Adrenergic Receptor
  4. AVN-101

AVN-101 is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis.

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AVN-101

AVN-101 構造式

CAS 番号 : 1025725-91-0

容量 価格（税別） 在庫状況 数量
5 mg $90 お問い合わせ 2 - 3 weeks 1 - 2 Weeks 3 - 4 weeks 2 - 3 weeks
10 mg $150 お問い合わせ 2 - 3 weeks 1 - 2 Weeks 3 - 4 weeks 2 - 3 weeks
25 mg $280 お問い合わせ 2 - 3 weeks 1 - 2 Weeks 3 - 4 weeks 2 - 3 weeks
50 mg $450 お問い合わせ 2 - 3 weeks 1 - 2 Weeks 3 - 4 weeks 2 - 3 weeks
100 mg $750 お問い合わせ 2 - 3 weeks 1 - 2 Weeks 3 - 4 weeks 2 - 3 weeks
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Other Forms of AVN-101:

AVN-101 関連抗体

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5-HT Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

Histamine Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

Adrenergic Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
α adrenergic receptor β adrenergic receptor

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製品説明

AVN-101 is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis[1].

IC50 & Target

5-HT2A Receptor

 

5-HT2C Receptor

 

5-HT6 Receptor

 

5-HT7 Receptor

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.158 μM
Compound: 4(2)
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
[PMID: 19945877]
SK-N-SH IC50
0.04 μM
Compound: 4(2)
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
[PMID: 19945877]
SK-N-SH IC50
0.146 μM
Compound: 4(2)
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
[PMID: 19945877]
体外実験

AVN-101 shows some ability to compete with radio-labeled ligands for both the histamine H1 (Ki  =  0.58 nM) and H2 receptors (Ki  =  89 nM) while being totally inactive on H3 receptor[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AVN-101 関連抗体
体内実験

AVN-101 (0.05 mg/kg; i.p.; once daily; for 4 days) reduces immobility in the forced swim test in mice[1].
AVN-101 (0.02-5 mg/kg; i.p.; once) prevents Scopolamine (HY-N0296)-induced amnesia in a passive avoidance test in mice when administered at a dose of 0.05 mg/kg[1].
AVN-101 (0.2, 1, and 5 mg/kg) increases the time spent in the open arms of the elevated plus maze in mice[1].
AVN-101 is poorly stable in murine plasma: by the end of 30-min incubation at room temperature, the residual amount of the original compound is reduced to 16%. At the same time, AVN-101 shows better stability in plasma samples taken from monkey and human: by the end of the 30-min incubation at room temperature, the residual amount of the original compound is reduced to only 45% and 68%, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/C mice bearing porsolt forced swim and the tail suspension tests[1].
Dosage: 0.05 mg/kg
Administration: i.p.; once daily; for 4 days
Result: Reduced immobility in the forced swim test in mice.
Animal Model: Male BALB/c mice were used with amnesiac models based on either Scopolamine-induced memory impairment[1].
Dosage: 0.02 mg/kg, 0.05 mg/kg, 0.2 mg/kg, 0.5 mg/kg, 1 mg/kg, and 5 mg/kg
Administration: i.p.; once
Result: Prevented scopolamine-induced amnesia in a passive avoidance test in mice
分子量

304.43

分子式

C21H24N2
CAS 番号
SMILES

CC1=CC2=C(N(CCC3=CC=CC=C3)C4=C2CN(C)CC4)C=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
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AVN-101 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AVN-1011025725-91-0AVN101AVN 1015-HT ReceptorHistamine ReceptorAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta Receptorbrain-penetrantorally active5-HT7 receptoranxiety disordersdepressionschizophreniaAlzheimer’s diseaseand multiple sclerosisInhibitorinhibitorinhibit

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製品番号:
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